Klimen - Instructions For Use, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Klymene

Klimen: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Drug interactions
11. 11. Analogs
12. 12. Terms and conditions of storage
13. 13. Terms of dispensing from pharmacies
14. 14. Reviews
15. 15. Price in pharmacies

Latin name: Climen

ATX code: G03CA53

Active ingredient: cyproterone + estradiol (cyproteronum + oestradiolum)

Producer: Delpharm Lille SaS (France)

Description and photo update: 2019-14-08

Prices in pharmacies: from 949 rubles.

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Klymen is an anti-climacteric agent with antiandrogenic, gestagenic and antigonadotropic action.

Release form and composition

Dosage form Klimen - two types of pills: white and pink (in a blister 11 pcs. White and 10 pcs. Pink pills, in a cardboard box 1 blister).

Content of active ingredients in 1 tablet:

• White: estradiol valerate - 2 mg;
• Pink: estradiol valerate - 2 mg, cyproterone acetate - 1 mg.

Auxiliary components: calcium carbonate, corn starch, lactose monohydrate, povidone 25,000 (K25), magnesium stearate, povidone 700,000 (K700), sucrose, macrogol 6000, wax, talc.

Additionally, in the composition of pink dragees: glycerol 85%, iron oxide yellow, iron oxide red, titanium dioxide.

Pharmacological properties

Pharmacodynamics

Klymene contains estrogen - estradiol valerate, which in the human body turns into the form of 17β-estradiol, similar to a substance synthesized by the ovaries. Also, the active ingredient is a progesterone derivative - cyproterone acetate, which is characterized by antiandrogenic, antigonadotropic and gestagenic effects.

Thanks to the active substances and the cyclic scheme of taking Klymen (for 11 days, only estrogen is taken, then estrogen and progestogen for 10 days, followed by a break for 7 days) in patients suffering from menstrual irregularities, with regular intake of the drug, menstrual recovery is observed cycle.

Against the background of the use of Klimen, there is no suppression of ovulation, and the synthesis of hormones in the body itself remains unchanged. It is allowed to use the drug in women of reproductive age in order to normalize the menstrual cycle, as well as in women with menstrual dysfunctions in the premenopausal period.

Estradiol eliminates the lack of estrogen in the female body during menopause and contributes to the effective treatment of autonomic and psychoemotional symptoms of menopause (these include joint and muscle pain, hot flashes, decreased libido, intense sweating, headache, dizziness, sleep disturbances, cardialgia, palpitations, increased nervous excitability, irritability), as well as involutions of the skin and mucous membranes, especially the mucous membranes of the genitourinary organs [pain during intercourse, irritation and dryness of the vaginal mucosa, enuresis (urinary incontinence)]. Estradiol prevents the decrease in bone mass, provoked by a lack of estrogen. This is mainly due to the suppression of the function of osteoclasts and the normalization of the balance between the processes of resorption and bone formation. Studies have shown that long-term use of hormone replacement therapy (HRT) leads to a decrease in the risk of peripheral bone fractures in patients who are in menopause. Withdrawal of HRT is accompanied by a decrease in bone mass, the rate of which is comparable to the parameters characteristic of the time interval immediately after the onset of menopause. The assumption that the appointment of HRT makes it possible to achieve restoration of bone mass to the value determined before menopause is considered unfounded.characteristic of the time interval immediately after the onset of menopause. The assumption that the appointment of HRT allows you to restore bone mass to the value determined before menopause is considered unfounded.characteristic of the time interval immediately after the onset of menopause. The assumption that the appointment of HRT allows you to restore bone mass to the value determined before menopause is considered unfounded.

HRT also has a beneficial effect on the concentration of collagen in the skin, as well as on its density, which makes it possible to slow down the formation of wrinkles. The antiandrogenic properties of cyproterone acetate provide a therapeutic effect on the body in androgen-dependent diseases (these include androgenetic alopecia, seborrhea, acne).

Taking Klymen leads to a decrease in the content of low-density lipoproteins (LDL) and total cholesterol and an increase in the level of high-density lipoproteins (HDL), as a result of which the ratio of HDL / LDL increases significantly, as well as an increase in the concentration of triglycerides. Since cyproterone acetate lacks androgenic properties, this substance practically does not change the degree of effect of estradiol on lipid metabolism. The results of treatment with Klymen are especially noticeable in patients with distinct atherogenic changes in the lipid profile.

Taking cyproterone acetate for 10 days during each cycle prevents the development of endometrial hyperplasia and oncological diseases.

Observations in the course of studies suggest that among postmenopausal patients, the use of HRT decreases the incidence of colon cancer. The mechanism of action is not well understood.

Pharmacokinetics

Estradiol valerate

When taken orally, estradiol valerate is absorbed almost completely and at a high rate. In the process of absorption and primary passage of the substance through the liver, the ester is split into valeric acid and estradiol. At the same time, estradiol is largely metabolized further, splitting into estrone, estrone sulfate and estriol. When taken orally, the bioavailability of estradiol is approximately 3%. This indicator is not affected by the simultaneous intake of Klymene with food.

The maximum level of estradiol in blood plasma is about 30 pg / ml and is reached 4-9 hours after taking Klymene. One day after administration, the content of estradiol in the blood plasma decreases to a concentration of about 15 pg / ml. Estradiol binds to sex hormone binding globulin (SHBG) and albumin. The free fraction of estradiol in blood plasma is approximately 1–1.5%, and the fraction of the compound bound by SHBG is in the range of 30–40%.

The apparent volume of distribution of the substance after a single intravenous administration reaches approximately 1 l / kg.

After the hydrolysis of estradiol valerate of exogenous origin, the compound is biotransformed in the same ways as endogenous estradiol. The metabolic processes of estradiol are carried out mainly in the liver, and also partially in the target organs, intestines, skeletal muscles and kidneys. As a result of these processes, catechol estrogens, estriol and estrone are formed, as well as glucuronide and sulfate conjugates of these compounds, which are characterized by significantly less estrogenic activity or not at all.

The clearance of estradiol from blood plasma after a single intravenous injection is characterized by a high degree of variability in the range of 10–30 ml / min / kg. Some of the estradiol is excreted together with bile and takes part in the intestinal-hepatic recirculation. Estradiol metabolites are excreted mainly in the urine in the form of glucuronides and sulfates.

The content of estradiol in blood plasma after repeated administration is approximately 2 times higher than after administration of a single dose. On average, the level of estradiol in the blood plasma ranges from 40 pg / L (minimum concentration) to 90 pg / L (maximum concentration). The content of estrone, which is a weaker estrogen, is approximately 8 times, and the content of estrone sulfate is approximately 150 times higher than that of estradiol. After the cancellation of Klymene, the concentrations of estrone and estradiol return to their original values for 2-3 days.

Cyproterone acetate

After oral administration of cyproterone acetate in a wide range of doses, the substance is rapidly and completely absorbed. Absolute bioavailability after oral administration reaches 88%.

The maximum concentration of this active component in blood plasma is approximately 30 ng / ml and is reached within 1-2 hours after a single dose of 1 mg of cyproterone acetate. After this, a two-phase decrease in the level of cyproterone acetate in blood plasma is noted, with the half-lives of 0.8 hours and 2.3 days, respectively.

Cyproterone acetate binds almost exclusively to serum albumin. Approximately 3.5–4% of the total concentration of the substance is contained in the blood plasma in unbound form. Due to the non-specificity of binding to blood plasma proteins, changes in the concentration of SHBG do not affect the pharmacokinetics of cyproterone acetate.

Metabolism of cyproterone acetate is carried out in various ways, including through conjugation and hydroxylation. The main metabolite found in human blood plasma is 15β-hydroxyl derivative.

Plasma clearance of cyproterone acetate is 3.6 ml / min / kg. A certain part of the administered dose is excreted unchanged in the bile. Most of the dose is excreted in the form of metabolites in the urine and faeces in a ratio of 3: 7. The half-life is 1.9 days. The metabolites are excreted from plasma with an identical half-life of 1.7 days.

Due to the prolonged half-life of cyproterone acetate from plasma, it can be assumed that the concentration of this substance in the blood plasma during one cycle of taking Klymene increases by 2–2.5 times.

Indications for use

According to the instructions, Klimen is indicated for women for the treatment and prevention of pathologies associated with hormonal disorders in the body:

• Menopausal disorders, involutional changes in the genitourinary tract and skin, symptoms of estrogen deficiency against the background of sterilization or primary ovarian dysfunction (with an unremoved uterus), hypogonadism or natural menopause, depressive conditions in the climacteric period - in the form of hormone replacement therapy;
• Irregular menstrual cycles;
• Amenorrhea (primary or secondary);
• Prevention of the development of postmenopausal osteoporosis.

Contraindications

The use of Klimen for hormone replacement therapy is contraindicated in women with the following diseases and conditions:

• Vaginal bleeding of unknown origin;
• Breast cancer (suspected or diagnosed);
• Malignant tumors or precancerous diseases of hormone-dependent etiology (presumptive diagnosis or confirmed);
• Severe forms of liver disease;
• Benign or malignant liver tumors (indicated in history or currently);
• Deep vein thrombosis (with exacerbation), thromboembolism (indicated in history or currently);
• Thromboembolism or acute arterial thrombosis, including myocardial infarction, stroke;
• Severe hypertriglyceridemia;
• The period of pregnancy and breastfeeding;
• Hypersensitivity to Klymene components.

If signs of these pathologies occur during the treatment period, you should immediately stop taking the pills.

It is recommended to prescribe the drug with caution to women with arterial hypertension, diabetes mellitus, congenital hyperbilirubinemia (Gilbert, Rotor and Dabin-Johnson syndrome), cholestatic jaundice or cholestatic itching during gestation, uterine myoma, endometriosis.

Instructions for the use of Klymene: method and dosage

Dragee is taken orally, without chewing, and washed down with a small amount of liquid. Klimen is taken once a day at a time convenient for the patient, which is mandatory for all subsequent pills.

For women with ongoing menstruation, the drug should be started on the 5th day of menstrual bleeding.

With amenorrhea, postmenopause, or very rare menstruation, you can start taking it at any time, provided that pregnancy is excluded.

Treatment should be started with white pills, 1 pill per day for 11 days, then 1 pink pill for 10 days. The course of one package is designed for a 21-day intake, followed by a 7-day break. During a break, a woman's menstrual bleeding occurs 2-3 days after taking the last tablet.

The first dragee from a new package should be taken after a 7-day break, on the same day of the week as from the previous package.

If at the set time a woman accidentally missed taking the next pill, it should be taken as soon as possible (12-24 hours). With a longer break between doses, vaginal bleeding may occur.

Side effects

The use of Klymene can cause side effects:

• On the part of the reproductive system and mammary glands: soreness, tension and / or enlargement of the mammary glands, bloody intermenstrual discharge, breakthrough bleeding, changes in the intensity and frequency of uterine bleeding (usually weakened during therapy), changes in vaginal discharge, dysmenorrhea, a condition similar premenstrual syndrome;
• From the gastrointestinal tract: nausea, abdominal pain, vomiting, dyspepsia, bloating, recurrence of cholestatic jaundice;
• From the nervous system: dizziness, headache, symptoms of depression, anxiety, migraine, increased fatigue;
• On the part of the skin and subcutaneous tissue: itching, skin rash, erythema nodosum, chloasma;
• Others: increased blood pressure, heart palpitations, thromboembolism and venous thrombosis, edema, muscle cramps, changes in libido, changes in body weight, contact lens intolerance, visual impairment, allergic reactions.

Overdose

If Klimen is accidentally taken at a dose that is many times higher than the recommended daily dose, the risk of serious side effects is considered minimal. There is no specific antidote, and symptomatic therapy is prescribed for a diagnosed overdose.

special instructions

The use of the drug is recommended only as directed by a doctor, after a thorough general medical and gynecological examination, confirmation of the absence of pregnancy and violations of the blood coagulation system.

When prescribing Klymene to women of age, with a genetic predisposition, severe obesity, the ratio of risk and benefit of therapy should be weighed.

The drug is not a contraceptive and is not intended to be used to prevent pregnancy.

If contraception is necessary, a woman should be advised to use non-hormonal drugs. If you suspect pregnancy, Klymene should be suspended until her absence is confirmed.

Against the background of hormone replacement therapy, the likelihood of developing venous thromboembolism increases, especially in patients with risk factors. During the period of prolonged immobilization or with extensive injuries, it is recommended to temporarily stop taking pills. If signs of thrombotic disorders appear, the use of Klymene should be canceled.

Long-term estrogenic monotherapy increases the risk of developing carcinoma or endometrial hyperplasia, the presence of gestagens - reduces the likelihood of cancer and endometrial hyperplasia.

The relative risk of developing breast cancer increases in women taking Clemen for several years.

Hormone therapy increases breast density on mammograms, which in some cases can interfere with X-ray detection of breast cancer.

Against the background of the use of sex steroids, in rare cases there are benign or malignant tumors of the liver, in some cases - with intra-abdominal bleeding. With an enlarged liver, pain in the upper abdomen, or diagnosed symptoms of intra-abdominal bleeding, the possibility of a liver tumor should be considered.

Estrogens potentiate the lithogenicity of bile; in predisposed women, this leads to the development of gallstone disease while taking pills.

If you experience very severe, frequent headaches or migraine-like conditions, you must stop treatment and make sure that they are not symptoms of a thrombotic cerebral stroke.

The use of hormonal drugs can cause a slight increase in blood pressure, which has no clinical consequences. With the development of persistent arterial hypertension, Klymene should be canceled.

Hormone replacement therapy in patients with impaired liver function should be carried out under regular medical supervision and periodic liver function tests. In case of deterioration of laboratory parameters or recurrence of cholestatic pruritus or jaundice, first observed during pregnancy or previous hormonal therapy, the use of Klymen should be discontinued.

In patients with a moderately elevated triglyceride content, taking pills contributes to an increase in their blood level and the risk of developing acute pancreatitis.

The use of a hormonal agent can cause uterine bleeding; with an increase in their frequency and abundance, it is necessary to conduct a study of the endometrium.

In the absence of normalization of menstrual cycles in the treatment of their irregularity, it is necessary to conduct additional examinations of the patient.

In case of recurrence of endometriosis, with an increase in uterine fibroids under the influence of estrogens, their use should be discontinued.

Treatment should be started after excluding the presence of prolactinoma.

Chloasma is more often observed in patients with a history of this disease. Women prone to its development should avoid prolonged ultraviolet radiation during the period of taking pills.

If a benign breast tumor, epilepsy, bronchial asthma, porphyria, migraine, systemic lupus erythematosus, otosclerosis, chorea minor occurs, the use of hormonal drugs should be supervised by the attending physician.

Reception of Klymen can affect the results of laboratory tests - indicators of carbohydrate metabolism, fibrinolysis, coagulation, biochemical indicators of the function of the adrenal glands, kidneys, liver, thyroid gland, the level of transport proteins in the blood plasma.

Klymen does not affect the patient's ability to drive vehicles and mechanisms.

Application during pregnancy and lactation

Reception of Klymene during pregnancy and breastfeeding is contraindicated. If the pregnancy test is positive, you should immediately stop taking the drug. Sex hormones in small concentrations can be excreted in breast milk.

Large-scale epidemiological studies of the effects on the body of steroid hormones used for HRT or contraception have not confirmed an increased risk of birth defects in newborns whose mothers took such hormones before pregnancy, as well as the presence of a teratogenic effect of hormones when they are accidentally taken in early pregnancy.

Drug interactions

The simultaneous use of Klimen with hormonal contraceptives is contraindicated.

Long-term use of certain antibiotics and anticonvulsants, including hydantoins, barbiturates, primidone, carbamazepine, rifampicin, and presumably oxcarbazepine, topiramate, felbamate, and griseofulvin, can induce liver enzymes, increasing the clearance of sex hormones and decreasing their clinical efficacy. Enzyme induction reaches a maximum usually after 2-3 weeks of using the drug and can persist for 4 weeks after discontinuation.

Against the background of the simultaneous administration of antibiotics of the tetracycline or penicillin group, a decrease in the level of estradiol is possible.

Paracetamol and other substances that undergo a significant degree of conjugation can increase the bioavailability of estradiol.

Klymen affects glucose tolerance, a dose adjustment of concurrent oral antidiabetic drugs or insulin may be required.

Drinking large doses of alcohol increases the level of estradiol in the blood.

Analogs

The analogues of Klymene are: Klimadinon, Klimadinon Uno, Tsi-Klim.

Terms and conditions of storage

Keep out of reach of children at room temperature.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Klymene

Mostly the reviews about Klymene, which are left by the patients, are positive. It allows you to eliminate neuroendocrine, neuropsychic and vegetative-vascular symptoms associated with a decrease in the production of estrogen by the ovaries. Also, the drug has a beneficial effect on the body with Alzheimer's disease, osteoporosis and coronary heart disease, as well as with urogenital disorders and changes in appearance associated with premature aging. At the same time, women note a rapid regression of autonomic symptoms and the effectiveness of Klimen in the prevention of various diseases that arise with age.

However, taking the drug has its drawbacks. These include a fairly high cost, a large number of contraindications and side reactions (edema, headache, increased blood pressure) and the need to gradually reduce the dose of estrogen in the event of Klymen's cancellation. It is often used in young women for hyperandrogenism, acne and hair loss. Klymen can only be prescribed by a doctor after a thorough general medical and gynecological examination: self-medication is unacceptable.

Price for Klimen in pharmacies

The approximate price for Klimen in pharmacies ranges from 1103 to 1311 rubles.

Klimen: prices in online pharmacies

Drug name Price Pharmacy

Klymen film-coated tablets 21 pcs. 949 RUB Buy

Klimen dragee 21 pcs. 1172 RUB Buy

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!